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. 2025 May-Jun;26(7-9):311-329.
doi: 10.1080/14622416.2025.2547565. Epub 2025 Aug 21.

The pharmacogenetics of rosuvastatin and implications for treatment: a systematic review

Eva González-Iglesias  1   2 , Jesús Novalbos  1 , Francisco Abad-Santos  1   2   3
Affiliations

The pharmacogenetics of rosuvastatin and implications for treatment: a systematic review

Eva González-Iglesias et al. Pharmacogenomics. 2025 May-Jun.

Abstract

Introduction: Rosuvastatin has become a good choice in the statin group because it has shown greater efficacy in reducing lipid levels than other statins, allowing patients to reach their therapeutic goal more quickly. To date, research has shown a broad relationship between the kinetics and efficacy of this drug and the phenotype of two transporters, OATP1B1 and BCRP, encoded by SLCO1B1 and ABCG2 genes. However, there are many other genes whose variation may also affect the treatment.

Objective: To conduct a systematic review including all information on the kinetics, measured by AUC and Cmax parameters; efficacy, by reduction in lipid levels and carotid intima-media thickness; and safety of rosuvastatin, by the occurrence of adverse events.

Methods: A search of the published literature was conducted in PubMed using the term "rosuvastatin AND pharmacogenetics" (PROSPERO code: CRD420251041953).

Results: A total of 37 articles were included, investigating 40 genes.

Conclusions: The importance of ABCG2 in drug kinetics and efficacy and of SLCO1B1 in kinetics is confirmed, as is the possible association of CYP3A5 with efficacy and safety and of APOC1 with efficacy. There are also positive results for other genes that should be studied further to confirm their association with rosuvastatin.

Keywords: ABCG2; APOC1; Rosuvastatin; SLCO1B1; adverse events; efficacy; kinetics; systematic review.

Plain language summary

Rosuvastatin is a drug that helps lower cholesterol and other blood fats. It’s more effective and works faster than other statins. Its function is mainly linked to two genes: SLCO1B1 and ABCG2. These genes control proteins that move the drug around the body. However, other genes may also influence how the drug works. We reviewed 37 studies examining 40 genes to determine their impact on how the body processes rosuvastatin, its effectiveness in lowering cholesterol, and its potential to cause side effects. Our findings confirmed the relevance of the ABCG2 and SLCO1B1 genes and revealed that others, such as CYP3A5 and APOC1, may also play a role.

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Conflict of interest statement

Francisco Abad-Santos has been a consultant or investigator in clinical trials sponsored by the following pharmaceutical companies: Abbott, Alter, Aptatargets, Chemo, Cinfa, FAES, Farmalíder, Ferrer, GlaxoSmithKline, Galenicum, Gilead, Italfarmaco, Janssen-Cilag, Kern, Moderna, MSD, Normon, Novartis, Servier, Silver Pharma, Teva, and Zambon. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

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